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• Antineoplastic drug

  The active ingredient of triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue, which is also known as decapeptyl, diphereline, triptorelin acetate, gonadorelin. It is an antineoplastic drug, whose pharmacological effects are same with goserelin, buserelin, and its structure is modified by natural molecular structure of the sixth L-glycine that is replaced by D-tryptophan to promote efficiency and prolong the plasmic half-life time, as well as enhance drug efficacy. After intramuscular injection, it initially stimulates the pituitary gland to release luteinizing growth hormone (LH) and follicle-stimulating hormone (FSH). When the pituitary over a long period of stimulation will be into the refractory period, that reduced the release of gonadotropin, leading to sex hormones reduction to castrate levels. These effects are reversible. Subcutaneous administration is rapidly absorbed, and Tmax is 15min, and the effect is maximum at 1h. The intramuscular injection of sustained release formulations can maintain the efficacy reaching 28d or more. It Clinically uses for the treatment of endometriosis, hormone-dependent prostate cancer, breast cancer, precocious puberty, as well as it may also be used as assisted reproductive technology. The main side effects of triptorelin are as follows: In the early stage of treatment of male, it can cause urinary disorders, breast swelling and pain, bone pain, and it may also cause hot flashes, loss of libido and impotence. It rarely cause gynecomastia, testicular atrophy, and sleep disorders. In the first week of treatment for children, girls will occur small amount of vaginal bleeding, which can be corrected by short-term additional therapy. During the treatment of women, hot flashes, bleeding or bleeding spots, vaginal dryness, headaches and weakness can occur. It can cause abdominal and (or) pelvic pain when it uses combination with gonadotropin. Since the concentration of estrogen reduces to the level of post-menopause, it can cause slight loss of trabecular bone matrix. Generally, after cessation of treatment six to nine months the adverse reations can return to normal. There may be irreversible amenorrhea after treatment in patients with endometriosis.
  The above information is edited by the chemicalbook of Kui Ming. ;

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